38 results about "Dasatinib" patented technology

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

According to the invention, a polymer prodrug is designed and prepared, and a dasatinib (DAS) and triphenylphosphine-adriamycin (TPP-DOX, TD) co-loaded nano-micelle is constructed; the preparation method has the advantages that 1) the optimal preparation process of the polymer micelle is determined by a single factor investigation method, namely the optimal nano-micelle is prepared by using a dialysis method and taking DMF (Dimethyl Formamide) as a solvent according to the mass ratio of a prodrug material to a carried drug being 15: 1, and the preparation method is simple and clear and is easy to industrialize; 2) the particle size is small and uniform, so that the nanoparticles can be enriched at a tumor part through an EPR effect; 3) the amphiphilic micromolecule prodrug improves the water solubility of DAS, improves the drug stability, has high drug loading capacity, and avoids adverse reactions possibly caused by carriers and auxiliary materials; and 4) the polymer nano-micelle co-loaded with the DAS and the TPP-DOX has good MMP-2 sensitive responsiveness, enhances the drug targeting delivery capability, has good blood compatibility and safety, improves the drug curative effect, reduces the toxic and side effects, and has a good tumor MDR reversing effect.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The invention belongs to the field of biological medicine, and particularly relates to a nano-drug based on chondroitin sulfate as well as a preparation method and application of the nano-drug. Chondroitin sulfate (CS) and dasatinib (DAS) are connected through a GFLG connexon responded by cathepsin B (CTSB) to prepare the prodrug CS-GFLG-DAS (CGD), the prodrug CS-GFLG-DAS (CGD) is used for reversing the phenotype of cancer-related fibroblasts and reducing the biosynthesis of extracellular matrixes, fibrotic tumors are efficiently treated, and a new perspective is provided for optimizing the application of immunotherapy in fibrotic tumors.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a dalcotinib pharmaceutical composition and a preparation method thereof.The dalcotinib pharmaceutical composition is prepared from, by weight, 10-30 parts of dalcotinib, 25-60 parts of lactose, 25-60 parts of microcrystalline cellulose, 1-15 parts of carboxymethyl starch sodium and 0.5-5 parts of magnesium stearate; the average particle size D50 of the lactose is greater than or equal to 120 microns. The dalcotinib composition disclosed by the invention is high in dissolution rate, quick in disintegration, good in fluidity, capable of avoiding sticking, good in dissolution rate stability and simple in preparation process.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib vanillic acid crystal form and a preparation method thereof, and in the dasatinib vanillic acid crystal form provided by the invention, the molar ratio of dasatinib to vanillic acid to water is 1: 1: 1. The dasatinib vanillic acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.

The invention belongs to the technical field of biological medicines, and discloses application of dasatinib in preparation of a medicine for promoting retina ganglion cell axon regeneration and dendritic repair. The research of the invention finds that dasatinib has the effect of promoting RGC axon regeneration and dendritic repair after optic nerve injury. When dasatinib is adopted for treatment, repair and regeneration of retinal ganglion cell axons and dendrites after optic nerve injury can be promoted, and the purpose of treating traumatic optic nerve injury is achieved.

The invention relates to an application of a dasatinib and quercetin pharmaceutical composition in preparation of a medicine for improving the outcome of elderly adverse pregnancy, belongs to the technical field of biological medicines, and particularly discloses an application of the dasatinib and quercetin pharmaceutical composition. The technical problem of placenta dysfunction caused by elderly pregnancy is solved. The dasatinib and the quercetin form the pharmaceutical composition, so that the autophagy activity of trophoblasts is promoted, DNA (deoxyribonucleic acid) damaged cells are eliminated, the adverse pregnancy outcome caused by the elderly is remarkably improved, the embryo absorption rate is reduced by about 10%, and the weight of a fetus is increased by about 20mg. The invention provides a new targeted intervention strategy for the outcome of elderly adverse pregnancy.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection. The compositions may be administered intact, or may be crushed prior to administration.

Combination therapies for use in the treatment of brain tumours, particularly glioma and embryonal brain tumours. Disclosed herein are pharmaceutical compositions comprising a complex of Panobinostat and a cyclodextrin, a second pharmaceutical agent, and a pharmaceutically acceptable excipient, diluent or carrier, in which the second pharmaceutical agent is Niclosamide, Dasatinib or Duvelisib. Associated methods of treatment and use are further disclosed.

Described herein are methods useful for the treatment of cancers in a canine subject with a pharmaceutical compositions comprising HDAC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. Also described herein are methods for identification of subjects with cancers that will benefit from administration of the pharmaceutical compositions comprising HIDAC inhibitors, Rapamycin, Dasatinib, Lapatinib, Trametinib, Vorinostat, Imatinib, Crizotinib, Sorafenib, and combinations thereof. In certain aspects, the methods described herein further comprise administering a therapeutically effective amount of at least one additional anti-cancer agent.

The application discloses a kind of synthesis method of dasatinib intermediate in the field of organic synthesis, with 2-aminothiazole-4-carboxylic acid as raw material, first and tert-pivaloyl chloride in situ generates mixed anhydride, further and 2-chloro-6-methylaniline condensation reaction occurs after, the compound 2 obtained is not separated directly hydrolyzed to obtain high-purity 2-amino-N-(2-chloro-6-methylphenyl) thiazole-5-formamide.Due to the mixed anhydride formed by tert-pivaloyl chloride has greater steric hindrance, and the further reaction of corresponding amine is conducive to the regioselectivity, and by-product tert-pivalic acid can be easily removed by post-treatment, so as to solve the disadvantages existing in the prior art, the unit operation involved in the whole preparation process is simpler, and the product purity and yield are higher, with good application prospect.

Methods for the treatment of cancer, including glioblastoma multiforme (GBM) and recurrent glioblastoma multiforme (RGBM). The method includes administering to a patient a plurality of extraneous antineoplastons and a plurality of targeted agents. The plurality of extraneous antineoplastons may include two or more antineoplastons selected from phenylacetylglutaminate sodium (PG), phenylacetylisoglutaminate sodium (iso-PG), and phenylacetate (PN). The plurality of targeted agents may include two or more agents selected from bevacizumab, pazopanib, sorafenib, dasatinib, and everolimus.

The present invention relates to combination therapies for treating KRas G12C cancers. In particular, the present invention relates to methods of treating cancer in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a combination of a Src-family kinase inhibitor and a KRAS G12C inhibitor of Formula (I), Formula I-A or Formula I-B, pharmaceutical compositions comprising a therapeutically effective amounts of the inhibitors, kits comprising the compositions and methods of use therefor.

Provided herein are methods for deactivation of effector cells, such as NK cells, including cells for adoptive cell therapy that are off-the-shelf cells. The deactivated cells may be cryopreserved following deactivation. The deactivated and cell may be expanded and / or activated prior to deactivation, and may or may not comprise a transgene, which may optionally encode a chimeric antigen receptor and / or T cell receptor. In certain embodiments, disclosed are methods for deactivation of NK cells comprising treatment with a kinase inhibitor, for example an mTOR inhibitor and / or a tyrosine kinase inhibitor, for example rapamycin and / or Dasatinib. Also provided herein are deactivated and cryopreserved NK cells, and methods of preparing and / or using the same for treatment of a subject in need thereof, for example treatment of a subject with cancer.

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

The present application relates to the m 6 Application of methylation level of A as glioma marker, the present application confirms the m 6 The methylation modification level is related to the prognosis condition of brain glioma, and the increase of methylation abundance and expression level means worse prognosis. In addition, the present application researches and confirms that the expression of lncRNA-WEE2-AS1 is related to the formation of drug resistance of anti-tumor drugs, and inhibiting the expression of the lncRNA helps to improve the resistance of dasatinib, and provides a feasible treatment scheme for the clinical targeted treatment of drug-resistant patients.

The present invention discloses a method for regulating CAR-T cells and its application. The present invention regulates CAR-T cells through tyrosine kinase inhibitors, thereby alleviating and treating immune-related toxicities that may occur after CAR-T cells are used for treatment. The regulation method of the present invention can regulate the expression of various cytokines related to CAR-T cell immunotoxicity, perform early intervention on related toxicities, reduce the incidence and mortality of severe toxicities, and thus improve the safety of CAR-T cells. Dasatinib in the regulation method used in the present invention is an anti-tumor drug that has been approved for clinical treatment and can be applied in the treatment of various cancers, enabling the reuse of old drugs and having great economic value.

To provide an amorphous solid dispersion ("ASD") comprising dasatinib, a pharmaceutical composition comprising ASD, and a method of treatment comprising administration of the pharmaceutical composition.SOLUTION: Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions can be used in methods of treating a proliferative disorder, such as cancer, or in methods of delivering dasatinib to a patient regardless of whether the patient is concurrently using a gastric acid reducing agent or the patient has an elevated gastric pH. The composition may be particularly suitable for patients suffering from achlorhydria or hypoacidity, or Helicobacter pylori infection.SELECTED DRAWING: Figure 7

This invention belongs to the field of biotechnology and relates to the application of an inhibitor blocking the TRIB3 / SRC interaction, alone or in combination with an SRC kinase inhibitor, in the preparation of drugs for the prevention or treatment of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. Specifically, it discloses an inhibitor that overcomes resistance to traditional small molecule drugs and targets tumor migration and stemness by blocking the TRIB3 / SRC interaction, and its application, alone or in combination with an SRC kinase inhibitor, in the preparation of drugs for the prevention or treatment of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. The amino acid sequence of the TRIB3 / SRC kinase inhibitor is listed in SEQ ID No. 1, and the SRC kinase inhibitor is Dasatinib. We found that this peptide can promote the degradation of TRIB3 and SRC, inhibit tumor migration and stemness, and inhibit tumor development and progression. Combined use with an SRC kinase inhibitor shows significant efficacy, and therefore it is applied in the preparation of drugs for the treatment and prevention of pancreatic cancer, breast cancer, liver cancer, and kidney cancer. The prepared drugs show significant efficacy in treating tumor diseases, with few toxic side effects and high safety, and have promising development prospects.

The present invention discloses a cell membrane nanoparticle and its preparation method and use. + T cells, cell membrane nanoparticles TaCD4M1-NP with ROS response. This nanoparticle can carry CD4 + T cells infiltrate the inflammatory site and rely on the membrane proteins of the cell membrane to achieve enrichment and retention in the inflammatory site, increase the drug concentration in the target site, and reduce toxic and side effects. By selecting a combination of anti-inflammatory drugs, methotrexate and dasatinib were selected for combined administration. The results showed that the combination had synergistic efficacy in various inflammatory models. Cell membrane nanoparticles loaded with MTX and DAS can effectively carry CD4 + T cells, which infiltrate inflammatory sites such as the colon in ulcerative colitis (UC) and the joints in rheumatoid arthritis (RA), significantly enhance the efficacy of drugs against UC and RA, providing a new approach for the treatment of inflammatory diseases.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib fumaric acid crystal form and a preparation method thereof, and in the dasatinib fumaric acid crystal form provided by the invention, the molar ratio of dasatinib to fumaric acid to methanol is 1: 1: 1. The dasatinib fumaric acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.

The invention discloses a dasatinib drug sensitivity gene marker combination and a drug sensitivity prediction system. A signal interaction network is constructed and key regulatory factors are identified by comprehensively analyzing a gene expression profile, a gene marker combination remarkably related to the drug sensitivity of the dasatinib is obtained, and a prediction model can be trained through the gene markers and used for accurately predicting the drug sensitivity of the dasatinib, so that a reliable basis is provided for personalized treatment, and the drug sensitivity of the dasatinib is accurately predicted. And reference is provided for clinical treatment decisions.

The present invention relates to the prevention or mitigation of adverse effects related to gene therapy, such as the formation of anti-drug antibodies. Specifically, the invention relates to the prevention or mitigation of such side effects using a tyrosine kinase inhibitor such as dasatinib.

Disclosed in the present specification are a composition for improving, enhancing, or restoring the function of pancreatic β cells aged by pregnancy and childbirth, and biomarkers for predicting or diagnosing the function of pancreatic β cells aged by pregnancy and childbirth. In one aspect, the composition of the present invention can effectively enhance the proliferation of pancreatic β cells aged by pregnancy, childbirth, and multiple births by containing dasatinib and quercetin, and the biomarkers of the present invention are used such that conditions caused by pregnancy, childbirth and multiple births, such as an increased cellular stress of pancreatic β cells, impaired cellular respiration and secretory function, or decreased cell proliferation capacity can be predicted or diagnosed.

The present invention relates to a composition for inducing the reprogramming of type 1 alveolar cells into type 2 alveolar cells, comprising dasatinib as an active ingredient. According to the present invention, by reprogramming AT1 cells into AT2 cells using dasatinib, it is possible to efficiently secure AT2 cells, which were difficult to obtain in sufficient numbers. Furthermore, it is expected that cells with physiological activity similar to actual tissues can be secured by reprogramming AT1 cells into AT2 cells within the organoid while culturing the organoid itself, rather than culturing single cells.

The application discloses a preparation method of a platelet membrane modified iron-tungsten-oxygen ternary compound nano-platform loaded with platinum nanoparticles, and a product and application thereof, and comprises the following steps: 1) synthesizing the iron-tungsten-oxygen ternary compound through an organic phase thermal decomposition method; 2) synthesizing platinum nanoparticles; 3) adsorbing a dasatinib drug and the platinum nanoparticles on the iron-tungsten-oxygen ternary compound to form FPD; 4) preparing nanoscale platelet membrane vesicles; 5) preparing E5 peptide modified platelet membrane vesicles; and 6) ultrasonically dispersing the FPD and the E5 peptide modified platelet membrane vesicles to obtain the nano-platform. The nano-platform can efficiently load the chemotherapeutic drug dasatinib, has good biological safety and no toxic side effects, can target in-situ and circulating tumor cells, and can combine photothermal action, photodynamic action and drug chemotherapy to play the roles of resisting in-situ breast cancer and preventing breast cancer lung metastasis. Meanwhile, the excellent CT and MRI imaging characteristics of the nano-platform can be used for monitoring in-vivo tumors and drug conditions.

The invention relates to the technical field of biological medicines, and provides a medical application of dasatinib combined with quercetin in a radiation rectal injury repairing medicine or a treatment medicine, including radiation proctitis or radiation rectal fibrosis and other physical injuries. The invention creatively discovers for the first time and proves that under the combined application of dasatinib and quercetin in a mass ratio of 1: (5-50), the expression of senescence markers (P16, P21 and SASP) in rectal tissues can be remarkably reduced, the secretion of proinflammatory factors (IL-6, TNF-alpha and IL-1beta) and fibrosis-related proteins (TGF-beta and collagen) can be reduced, and the anti-aging effect of the dasatinib and quercetin is improved. The traditional Chinese medicine composition can play a therapeutic role by removing radiation-induced senescent cells, inhibiting intestinal inflammatory response, reducing fibrosis and promoting mucous membrane repair. A brand new strategy is provided for prevention and treatment research and drug development of radiation rectal injury after pelvic tumor radiotherapy, and the application has important clinical application significance.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dasatinib maleic acid crystal form and a preparation method thereof, and in the dasatinib maleic acid crystal form provided by the invention, the molar ratio of dasatinib to maleic acid to methanol is 1: 1: 1. The dasatinib maleic acid crystal form provided by the invention has relatively good stability and relatively high dissolution rate, and is of great significance for improving the bioavailability of a dasatinib medicine and preparing a preparation.